The effect of the putative endogenous imidazoline receptor ligand, clonidine-displacing substance, on insulin secretion from rat and human islets of Langerhans.

abstract：:1 The effects of diltiazem on smooth muscle cells of the canine basilar artery were investigated by means of microelectrode, double sucrose gap and isometric tension recording methods. 2 The mean membrane potential of the smooth muscle cells was -49.8 mV and they were electrically quiescent. Diltiazem (over 10(-5) M) ...

journal_title：British journal of pharmacology

authors： Fujiwara S,Ito Y,Itoh T,Kuriyama H,Suzuki H

更新日期：1982-03-01 00:00:00

abstract：:1. The potential influences of nitric oxide (NO) and prostaglandins on the renal effects of angiotensin II (Ang II) have been investigated in the captopril-treated anaesthetized rat by examining the effect of indomethacin or the NO synthase inhibitor, N(omega)-nitro-L-arginine methyl ester (L-NAME), on the renal respo...

journal_title：British journal of pharmacology

authors： Clayton JS,Clark KL,Johns EJ,Drew GM

更新日期：1998-08-01 00:00:00

abstract：:1. The effects of prejunctional beta-adrenoceptor activation on electrically evoked noradrenaline (NA) and adenosine 5'-triphosphate (ATP) were studied by use of continuous amperometry and conventional intracellular recording techniques. Excitatory junction potentials (e.j.ps) were used as a measure of ATP release, an...

journal_title：British journal of pharmacology

authors： Brock JA,Bridgewater M,Cunnane TC

更新日期：1997-03-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Endocannabinoids play an important role in modulating spinal nociceptive signalling, crucial for the development of pain. The cannabinoid CB1 receptor and the TRPV1 cation channel are both activated by the endocannabinoid anandamide, a product of biosynthesis from the endogenous lipid precursor N...

journal_title：British journal of pharmacology

authors： Nerandzic V,Mrozkova P,Adamek P,Spicarova D,Nagy I,Palecek J

更新日期：2018-06-01 00:00:00

abstract：:Melatonin receptors are seven transmembrane-spanning proteins belonging to the GPCR superfamily. In mammals, two melatonin receptor subtypes exist - MT1 and MT2 - encoded by the MTNR1A and MTNR1B genes respectively. The current review provides an update on melatonin receptors by the corresponding subcommittee of the I...

journal_title：British journal of pharmacology

authors： Jockers R,Delagrange P,Dubocovich ML,Markus RP,Renault N,Tosini G,Cecon E,Zlotos DP

更新日期：2016-09-01 00:00:00

abstract：:1. Repeated allergen challenge has been shown to increase the role of Rho-kinase in airway smooth muscle (ASM) contraction. We considered the possibility that active allergic sensitization by itself, that is, without subsequent allergen exposure, could be sufficient to enhance Rho-kinase-mediated ASM contraction. 2. G...

journal_title：British journal of pharmacology

authors： Schaafsma D,Gosens R,Bos IS,Meurs H,Zaagsma J,Nelemans SA

更新日期：2004-10-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Some neurosteroids, notably 3alpha-hydroxysteroids, positively modulate GABA(A) receptors, but sulphated steroids negatively modulate these receptors. Recently, other lipophilic amphiphiles have been suggested to positively modulate GABA receptors. We examined whether there was similarity among t...

journal_title：British journal of pharmacology

authors： Chisari M,Shu HJ,Taylor A,Steinbach JH,Zorumski CF,Mennerick S

更新日期：2010-05-01 00:00:00

abstract：:1 The effect of 5-hydroxytryptamine (5-HT) on acid secretion by a rat isolated stomach preparation has been studied. 2 5-HT at 10(-5)M in the serosal bathing fluid produced significant inhibition of the acid secretory responses to histamine, pentagastrin and isoprenaline but was without effect on basal secretion or th...

journal_title：British journal of pharmacology

authors： Canfield SP,Spencer JE

更新日期：1983-01-01 00:00:00

abstract：:1. The modulation by alpha 2-adrenoceptors of the jaw-opening reflex (digastric electromyographic responses) elicited by orofacial electrical stimulation (OF-JOR) in pentobarbitone anaesthetized rats was investigated. 2. Increasing doses of clonidine (0.1-1000 micrograms kg-1, i.v.) reduced, in a dose-dependent manner...

journal_title：British journal of pharmacology

authors： García-Vallejo P,Barturen F,García-Sevilla JA

更新日期：1994-04-01 00:00:00

abstract：:1. The pathological features of Gram-positive shock can be mimicked by the co-administration of two cell wall components of Staphylococcus aureus, namely lipoteichoic acid (LTA) and peptidoglycan (PepG). This is associated with the expression of the inducible isoform of nitric oxide synthase (iNOS) in various organs. ...

journal_title：British journal of pharmacology

authors： Kengatharan KM,De Kimpe SJ,Thiemermann C

更新日期：1996-12-01 00:00:00

abstract：:The effect of the selective serotonin reuptake inhibitor fluoxetine was examined on the 5-HT4 receptor-mediated relaxation in the rat isolated ileum. Fluoxetine unsurmountably antagonized the relaxation to exogenous 5-HT with abolition of the response at 10 microM. Fluoxetine (10 microM) also caused a gradual loss of ...

journal_title：British journal of pharmacology

authors： Tuladhar BR,Costall B,Naylor RJ

更新日期：2002-05-01 00:00:00

abstract：:Bradykinin, angiotensin II, arginine vasopressin (AVP) or des-amino-D-arginine vasopressin (DDAVP) were administered by intravenous infusion to 10 healthy men. The concentration of 6-oxo-prostaglandin F1 alpha (6-oxo-PGF1 alpha), the stable hydrolysis product of prostacyclin (PGI2), was measured in plasma using gas ch...

journal_title：British journal of pharmacology

authors： Barrow SE,Dollery CT,Heavey DJ,Hickling NE,Ritter JM,Vial J

更新日期：1986-01-01 00:00:00

abstract：:Mouse spiders represent a potential cause of serious envenomation in humans. This study examined the activity of Missulena bradleyi venom in several in vitro preparations. Whilst female M. bradleyi venom at doses up to 0.05 microl ml(-1) failed to alter twitch or resting tension in all preparations used, male venom (0...

journal_title：British journal of pharmacology

authors： Rash LD,Birinyi-Strachan LC,Nicholson GM,Hodgson WC

更新日期：2000-08-01 00:00:00

abstract：:RSD 921 is a novel, structurally unique, class I Na+ channel blocking drug under development as a local anaesthetic agent and possibly for the treatment of cardiac arrhythmias. The effects of RSD 921 on wild-type heart, skeletal muscle, neuronal and non-inactivating IFMQ3 mutant neuronal Na+ channels expressed in Xeno...

journal_title：British journal of pharmacology

authors： Pugsley MK,Goldin AL

更新日期：1999-05-01 00:00:00

abstract：:1. The neurotransmitters involved in NANC relaxation and their possible interactions were investigated in mouse isolated stomach, recording the motor responses as changes of endoluminal pressure from whole organ. 2. Field stimulation produced tetrodotoxin-sensitive, frequency-dependent, biphasic responses: rapid trans...

journal_title：British journal of pharmacology

authors： Mulè F,Serio R

更新日期：2003-09-01 00:00:00

abstract：:We investigated the action of the phenylalkylamines verapamil and N-methyl-verapamil on the Kv1.3 potassium channel using the whole-cell configuration of the patch-clamp technique. Our goal was to identify their binding as a prerequisite for using the phenylalkylamines as small, well-defined molecular probes, not only...

journal_title：British journal of pharmacology

authors： Rauer H,Grissmer S

更新日期：1999-07-01 00:00:00

abstract：:1. The effects of the glycine/NMDA receptor antagonist, (+)-HA-966 on the neurochemical and behavioural responses to amphetamine have been determined in the mouse and rat. 2. In vehicle-treated control mice, (+)-HA-966 (30-100 mg kg-1) did not affect dopamine synthesis in either the nucleus accumbens or striatum and w...

journal_title：British journal of pharmacology

authors： Hutson PH,Bristow LJ,Thorn L,Tricklebank MD

更新日期：1991-08-01 00:00:00

abstract：:1. Neurogenic responses to transmural electrical stimulation were examined in endothelium-denuded extrameningeal (vertebral and carotid) and intrameningeal (spinal, basilar and middle cerebral) arteries isolated from dogs. 2. In the extrameningeal arteries, transmural electrical stimulation produced a phasic contracti...

journal_title：British journal of pharmacology

authors： Kohno Y,Saito T,Saito H,Aoyama H,Nojyo Y,Kigoshi S,Muramatsu I

更新日期：1995-11-01 00:00:00

abstract：:The effects of 10 mM caffeine (CAF) on intramembrane charge movements (ICM) were studied in isolated guinea-pig ventricular heart cells with the whole-cell patch-clamp technique. In the presence of CAF, the properties (voltage dependence, maximum Q(ON) [Q(max)], availability with voltage) of Q(ON) charge activated fro...

journal_title：British journal of pharmacology

authors： Leroy J,Lignon JM,Gannier F,Argibay JA,Malécot CO

更新日期：2002-02-01 00:00:00

abstract：:1. The present study was aimed at elucidating the apoptosis inhibitory properties of the cyanoguanidine CHS 828. CHS 828 exhibits impressive cytotoxic activity in vitro and in vivo. Apoptosis is not its main mode of cytotoxic effect, and we have previously proposed a dual mechanism, where CHS 828 inhibits its own cell...

journal_title：British journal of pharmacology

authors： Martinsson P,Ekelund S,Nygren P,Larsson R

更新日期：2002-10-01 00:00:00

abstract：:1. The effect of 1-aminocyclopropanecarboxylic acid (ACPC), a partial agonist at the glycine site of the N-methyl-D-aspartate (NMDA) receptor complex that exhibits neuroprotective, anxiolytic and antidepressant-like actions, was investigated in a functional assay for presynaptic NMDA receptors. 2. NMDA (100 microM) pr...

journal_title：British journal of pharmacology

authors： Clos MV,Garcia Sanz A,Trullas R,Badia A

更新日期：1996-06-01 00:00:00

abstract：:1. In some asthmatics, muscarinic receptor antagonists are effective in limiting bronchoconstrictor response, suggesting an abnormal cholinergic drive in these subjects. There is a growing body of evidences indicating that cholinergic neurotransmission is also enhanced by endothelin-1 (ET-1) in rabbit bronchi, mouse t...

journal_title：British journal of pharmacology

authors： D'Agostino B,Advenier C,Falciani M,Gallelli L,Marrocco G,Piegari E,Filippelli A,Rossi F

更新日期：2001-12-01 00:00:00

abstract：:Ligands targeting GPCRs can be categorized according to their intrinsic efficacy to trigger a specific, receptor-mediated response. A ligand endowed with the same level of efficacy as the endogenous agonist can be classified as a full agonist, whereas a compound that displays greater efficacy, that is, higher receptor...

journal_title：British journal of pharmacology

authors： Schrage R,De Min A,Hochheiser K,Kostenis E,Mohr K

更新日期：2016-10-01 00:00:00

abstract：BACKGROUND:5-HT(2B) receptors are localized within the myenteric nervous system, but their functions on motor/sensory neurons are unclear. To explore the role of these receptors, we further characterized the 5-HT(2B) receptor antagonist RS-127445 and studied its effects on peristalsis and defecation. EXPERIMENTAL APPR...

journal_title：British journal of pharmacology

authors： Bassil AK,Taylor CM,Bolton VJ,Gray KM,Brown JD,Cutler L,Summerfield SG,Bruton G,Winchester WJ,Lee K,Sanger GJ

更新日期：2009-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The development of subtype-selective ligands to inhibit voltage-sensitive sodium channels (VSSCs) has been attempted with the aim of developing therapeutic compounds. Tetrodotoxin (TTX) is a toxin from pufferfish that strongly inhibits VSSCs. Many TTX analogues have been identified from marine an...

journal_title：British journal of pharmacology

authors： Tsukamoto T,Chiba Y,Wakamori M,Yamada T,Tsunogae S,Cho Y,Sakakibara R,Imazu T,Tokoro S,Satake Y,Adachi M,Nishikawa T,Yotsu-Yamashita M,Konoki K

更新日期：2017-11-01 00:00:00

abstract：:1. [Phe1psi(CH2-NH)Gly2]nociceptin-(1 - 13)-NH2 (Phepsi), a tridecapeptide analogue of orphanin FQ/nociceptin (OFQ/N), was introduced as a competitive antagonist of opioid receptor-like orphan receptor (ORL1) in guinea-pig ileum and mouse vas deferens preparations in vitro but was recently found to act as an agonist i...

journal_title：British journal of pharmacology

authors： Chiou LC

更新日期：1999-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:2-Hydroxypropyl-β-cyclodextrin (HPCD) is an FDA approved vehicle for drug delivery and an efficient cholesterol-lowering agent. HPCD was proposed to lower tissue cholesterol via multiple mechanisms including those mediated by oxysterols. CYP27A1 and CYP46A1 are the major oxysterol-producing enzym...

journal_title：British journal of pharmacology

authors： El-Darzi N,Mast N,Petrov AM,Pikuleva IA

更新日期：2020-07-22 00:00:00

abstract：:The effect of nicotine on the bioformation of prostacyclin (PGI2) and of thromboxane (Tx)B2 in rabbit aorta and platelets, respectively, was investigated. Rabbit aortic rings were incubated with [14C]-arachidonic acid ( [14C]-AA) and the incubation products were separated with thin layer chromatography (t.l.c.). Alter...

journal_title：British journal of pharmacology

authors： Alster P,Wennmalm A

更新日期：1984-01-01 00:00:00

abstract：:1. The aim of this study was to investigate whether the hypotensive effect of rat alpha-calcitonin gene-related peptide (alpha CGRP) in conscious rats is mediated by endothelium-derived nitric oxide (NO) or the opening of adenosine 5'-triphosphate (ATP)-sensitive potassium (KATP) channels. 2. Dose-mean arterial pressu...

journal_title：British journal of pharmacology

authors： Abdelrahman A,Wang YX,Chang SD,Pang CC

更新日期：1992-05-01 00:00:00

abstract：:The effects of caffeine and procaine on noradrenergic transmission in the guinea-pig mesenteric artery were investigated by recording electrical responses of smooth muscle cells and by measuring the outflow of noradrenaline (NA) and 3,4-dihydroxyphenylglycol (DOPEG) induced by perivascular nerve stimulation. Caffeine ...

journal_title：British journal of pharmacology

authors： Fujii K,Miyahara H,Suzuki H

更新日期：1985-03-01 00:00:00